2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. PNU-142633

PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy.

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PNU-142633

PNU-142633 構造式

CAS 番号 : 187665-65-2

容量 価格（税別） 在庫状況 数量
1 mg $165 在庫あり
5 mg $410 在庫あり
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50 mg   お問い合わせ  

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PNU-142633 関連抗体

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5-HT Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

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製品説明

PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy[1][2].

IC50 & Target[1]

5-HT1B Receptor

 

5-HT1D Receptor

 

5-HT1D Receptor

6 nM (Ki)

体外実験

The intrinsic activity of PNU-142633 at the human 5-HT1D receptor is determined to be 70% that of 5-HT in a cytosensor cell-based assay compared with 84% for that of Sumatriptan[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PNU-142633 関連抗体
体内実験

PNU-142633 (0.03-1 mg/kg; intravenous injection; male Hartley guinea pigs) treatment blocks neurogenic plasma protein extravasation. And PNU-142633 fails to alter resistance in these vascular beds[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Hartley guinea pigs (250-300 g) stimulated with bipolar electrode[1]
Dosage: 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg
Administration: Intravenous injection
Result: Significantly reduced extravasation at the 0.1 and 0.3 mg/kg doses, but was without effect at the 0.03 and 1.0 mg/kg doses.
分子量

422.52

分子式

C24H30N4O3
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C2C(CCO[C@H]2CCN3CCN(C4=CC=C(C(N)=O)C=C4)CC3)=C1)NC
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 42 mg/mL (99.40 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3668 mL 11.8338 mL 23.6675 mL
5 mM 0.4734 mL 2.3668 mL 4.7335 mL
10 mM 0.2367 mL 1.1834 mL 2.3668 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

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体積 （開始）

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3668 mL 11.8338 mL 23.6675 mL 59.1688 mL
5 mM 0.4734 mL 2.3668 mL 4.7335 mL 11.8338 mL
10 mM 0.2367 mL 1.1834 mL 2.3668 mL 5.9169 mL
15 mM 0.1578 mL 0.7889 mL 1.5778 mL 3.9446 mL
20 mM 0.1183 mL 0.5917 mL 1.1834 mL 2.9584 mL
25 mM 0.0947 mL 0.4734 mL 0.9467 mL 2.3668 mL
30 mM 0.0789 mL 0.3945 mL 0.7889 mL 1.9723 mL
40 mM 0.0592 mL 0.2958 mL 0.5917 mL 1.4792 mL
50 mM 0.0473 mL 0.2367 mL 0.4734 mL 1.1834 mL
60 mM 0.0394 mL 0.1972 mL 0.3945 mL 0.9861 mL
80 mM 0.0296 mL 0.1479 mL 0.2958 mL 0.7396 mL
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PNU-142633 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PNU-142633187665-65-2PNU142633PNU 1426335-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT1Danti-migraineplasmaproteinextravasationInhibitorinhibitorinhibit

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製品名:
PNU-142633
製品番号:
HY-103131
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